Radiodifluoromethylation of well-functionalized molecules

功能化分子的放射性二氟甲基化

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Abstract

The strategic installation of a [(18)F]fluorine atom at the specific position of the lead molecule is a never-ending challenge for radiochemists in their endeavour to develop novel positron emission tomography (PET) imaging applications. Although the radiosynthesis of [(18)F]CF(2)H-containing molecules has been explored in the past decade, more methods need to be explored for various well-functionalized compounds. Recently, two novel strategies of radiodifluoromethylation were reported, namely the utilization of [(18)F]difluorocarbene building block and frustrated Lewis pair-mediated C-(18)F bond formation, respectively. These methods provide an efficient radiofunctionalization of complex CF(2)H-containing molecules for drug discovery and PET ligand development.

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